All of Neuro drugs!!

Treatments for acute Migraines

Triptans (affect the serotonin system); behavioral adjustments (keep a journal of what you eat and try to avoid certain foods for the future)

NSAIDS

Sitans

Gepants

Ergots

Ergots

Ergotamine (± caffeine)

Dihydroergotamine (DHE)

Use

- Moderate/severe migraines

- Cluster HAs

- short term only (2-3 wks)

Gepants

Rimegepant

Ubrogepant

Ditans

Lasmiditan

Triptans

Sumatriptan

Naratriptan

Eletriptan

Zolmitriptan

Rizatriptan

Almotriptan

Frovatriptan

Excedrin

acetaminophen, aspirin, caffeine

MOA of Excedrin

decrease PGs, increase pain threshold, increase drug efficacy

Which drug is approved for the acute treatment of moderate to severe migranes?

Triptans

When is the most effective time to use a triptan?

Most effective when used early (

Which two triptans are used for the acute cluster headaches?

Sumatriptan (injectable) and zolmitriptan (nasal spray)

What prevents migraine attacks in woman during menstrual periods?

Triptans

MOA of triptans?

1. 5-HT1b agonist

2. 5-HT1d agonist

-- peripheral effect causing a decrease in vasodilation.

--central effect--decrease pain and neurogenic inflammation

What triptan overcomes first pass metabolism?

And what is a side effect?

Nasal Spray

GI upset and CNS depression

What is the first oral "ditans"

Lasmiditan--treatment of acute migraines in adults

What are the receptors of the ditans?

5HT1F

Do the ditans have peripheral or central effects?

Central effects--decreases pain and neurogenic inflammation

Does Lasmiditan cause vasoconstriction?

NO

CNS depressants and alcohol effects with Lasmiditan?

increases risk of sedation

Can Lasmiditan increase 5-HT--serotonin syndrome??

yes

Rimegepant is the only medication used for?

For acute and chronic migraines

What drug is used when triptans fail to work?

Gepants

Gepants antagonists block what?

CGRP receptors in sensory nerves decreasing pain and inflammation

What is increased during migraine attacks inducing pain and inflammation?

Calcitonin gene-related peptide

Where is Gepants metabolized?

liver

Can you use Gepants with overuse headache disorders?

NO

What drug is used for cluster headaches--and are not effective for tension headache

Ergots

CAN YOU USE ERGOTS WHILE PREGNANT???

NO!

What is considered a chronic migraine?

greater/equal to 15 days per month for 3 months

Non-migrane specific drugs

beta blockers

antiepileptics

what beta blockers are approved for prevention of chronic migraine?

Propranolol and metoprolol

What antiepileptics are used to prevent chronic migrane?

Valproate and Topiramate

What antiepileptic medication is associated adverse fetal events?

Valproate

What anti-cgrp receptor is approved for the treatment of episodic cluster headache?

Galcanezumab

Name 3 drugs that block CGRP receptors in sensory nerves decreasing pain and inflammation?

Erenumab

Galcanezumab

Fremanezumab

What headache medicine is used in IV infusions per year

Eptinezumab

What is the MOA of eptinezumab?

is an anti-calcitonin gene-related peptides

Local anesthetics

esters and amides

Esters "one eyed ester"

procaine, benzocaine, choloroprocaine, cocaine

Amides

Lidocaine (Xylocaine)

Bupivacaine (marcaine)

Etidocaine (duranest)

Prilocaine (Citanest)

Ropivacaine (Naropin)

MOA of local anesthetics

Bind to and block activated sodium channels in the inner portion of the channel

Can you take a local anesthetics with a vasoconstrictor (such as epinephrine)?

Yes--it enhances the block duration of action by decreasing systemic absorption

Which one has less allergic effects--amides or esters?

amides

What causes rapid breakdown of esters?

plasma esterases

What hydrolyzes esters?

plasma cholinesterases

What drug can cause methemoglobinemia?

Prilocaine

What are blocked first with Local Anesthetics?

unmyelinated nerve pain fibers (A delta, C fibers) blocked first

Adverse effects of Local Anesthetics?

CNS excitation--stimulation, Hypotension bc of vasodilation, cardiac depression, seizures and coma--bc of respiratory depression

Clinical uses of local anesthetics

Topical (itching)

sprays (ENT)

hemorrhoids

Spinal interathecal anesthesia--where do you inject the local anethestic?

into the subarchnoid space

Which ester is used for topical use?

benzocaine

What is the most common clinically selective opioid?

mu opioid receptor

Opioid Antangonists

Naloxone

Naltrexone

Methylnaltrexone

Opioid Analgesics

Morphine

Methadone

Meperidie

Oxycodone

Fentanyl

Hydrocodone

Codeine

Tramadol

Buprenophine

MOA of opioid agonists

Inhibit release of ACh, norepinehphrine, 5-HT, glutamate

Modulates synaptic transmission

Which opioid analgesics is a partial agonist?

buprenorphine

CNS effects of opioid anagelsics

pain relief without loss of consciousness

CNS depression with other drugs

can be abused because of the release of dopamine

euphoria or dysphoria

miosis (pinpoint pupils)

reduces responsiveness of medulla to CO2

cough suppression

Nausea, vomiting--direct stimulation of chemoreceptor trigger zone (CTZ)

What are the peripheral effects of opioids?

cardiovascular system--vasodilation--release of histamine from mast cells

cardiac effects--decreases oxygen demand, cardiac work

constipation

increase pressure of biliary tract--constriction of sphincter of Oddi

Can opioids prolong labor?

yes

What is causing the pruritis?

histamine release

Which opioid partial agonist decreases the chances of overdose?

Buprenorphine

Morphine

Moderate to severe pain--patient not responding to NSAIDS

large first pass effect and active metabolite

What is the treatment for a heroin addict?

Methadone

Can you use Meperidine in a pregnant patient?

Yes

Which opioid analgesic is commonly used with NSAIDS?

oxycodone

Tramadol

Inhibits the reuptake of norepinephrine and serotonin

AE: decreases seizure threshold and 5-HT syndrome

Different ways of receiving buprenorphine

transdermal patch, rods for implant, sublingual tract, a buccal film

Which opioid is used to prevent relapse?

Nalxone--"to save a life"

Signs of opioid overdose and treatment

miosis, respiratory depression and coma

Which opioid analgesic can be used to reverse tonic-clonic seizures?

naloxone

Which Antiepileptc drug can cause a neural tube defect?

Valproic Acid

Teratogens

agents, such as chemicals and viruses, that can reach the embryo or fetus during prenatal development and cause harm

Toxic effects of drugs on the placenta is what kind of effect?

A direct toxicant exposure

New system for classifying drug safety during pregnancy

narrative section:

-pregnancy exposure registry, risk summary, data

-lactation-risk summary, clinical consideration, data

-pregnancy test, contraception

Outcomes following exposure to drugs (mom to baby)

language and social deficits

cognitive and executive dysfunctions

mood dysfunction and autonomic arousal

multisensory functional and perceptual deficits

Drugs affecting neurodevelopment

thalidomide

misoprostol

Antiepiletic drugs (phenytoin, valproate, carbamazepine)

coumarin derivatives

retinoid class

Abused drugs/substances (eg-cocaine, morphine, alc)

Alcohol can cause what kind of deficiency?

Zn

Cyclophosphamide

alkylating agent chemotherapeutic agent

environmental factors

heavy metals (leads, mercury, cadmium, arsenic)

Polychlorinate biphenyls

persticides

What can you give mom to help with neurodevelopment?

Folic acid supplements

Thalidomide

Limb defects (flipper limbs)

inhibits ubiquitin ligase activity

A mechanism that is involved in a teratogenic response?

Oxidative stress/free radicals--interfere with DNA and RNA function

Levodopa

Dopamine precursor: used in parkinsonism, usually combined with carbidopa (a peripheral inhibitor of dopamine metabolism).

Toxic effect of levodopa

dyskinesias, hypotension, on−off phenomena, behavioral changes

COMT inhibitors

Entacapone

Tolcapone

Opicapone

COMT inhibitors are important for what kind of episodes?

"Wearing off"

Tolcapone (on the exam)

Crosses the BBB--increases brain levels of levodopa--decreases the metabolosm of levodopa

Can you used tolcapone in person with liver problems?

No! It can cause heptatic impairment

MAO-B inhibitors MOA

Inhibits MAO-B (in the brain) which degrades dopamine--increasing the brain dopamine

causing an increase in the concentration of dopamine

Amantadine

monotherapy--for early or advanced PD in adults

TREMORS

can use this for long term use (1-2 years)

promotes DA release from the presynaptic neurons

What drug is the best for tremors?

Amantadine

Can you use Amantadine with a pt with renal impairment?

no

Side effects of amantadine

Anticholinergic effects--dry mouth, GI upset, urinary retention

CNS depression

hypotension, hallucination

Dopamine receptor agonists

ropinirole, pramipexole, rotigotine, apomorphine

can you use dopamine agaonist as a monotherapy?

yes! in early stages of PD

Which dopamine receptor do we stimulate with a dopamine agonist?

D1-3

Does Levodopa replace dopamine?

yes

The most important MOA of repoinirole consist in___

dopamine receptor

What drugs increase dopamine content in the brain?

levodopa and carbidopa

What drugs decrease carbidopa and DA catabolism?

COMT inhibitors

What drugs ONLY decrease DA catabolism?

MAO-B inhibitors